β-Secretase Inhibitor IV
Based on 1 Customer Validation
β-Secretase Inhibitor IV is a potent, cell-active BACE-1 inhibitor with IC50s of 15.6 and 16.3nM under BACE-1 concentrations of 2 nM and 100 pM, respectively.
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- Pureté: 99.19%
- CAS No.: 797035-11-1
- Formule: C31H38N4O5S
- Masse moléculaire:578.72
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Stockage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
IC50: 15.3±0.6 nM (BACE-1), 230±26 nM (BACE-2), 7620±210 nM (Cathepsin D)[1]
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Cell Line
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Type | Value | Description | References |
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| CHO | IC50 |
0.078 μM
Compound: 24
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Inhibition of memapsin 2 expressed in CHO cells
Inhibition of memapsin 2 expressed in CHO cells
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[PMID: 17432843] |
| CHO | IC50 |
4.5 x 10-8 M
Compound: IV
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Inhibition of recombinant human BACE1 expressed in CHO cells co-transfected with human APP with Swedish mutation assessed as amyloid beta1-40 secretion by alphaLISA technique
Inhibition of recombinant human BACE1 expressed in CHO cells co-transfected with human APP with Swedish mutation assessed as amyloid beta1-40 secretion by alphaLISA technique
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[PMID: 22225636] |
| CHO | IC50 |
4.5 x 10-2 μM
Compound: IV
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Inhibition of recombinant human BACE1 expressed in CHO cells co-transfected with human APP with Swedish mutation assessed as amyloid beta1-40 secretion by alphaLISA technique
Inhibition of recombinant human BACE1 expressed in CHO cells co-transfected with human APP with Swedish mutation assessed as amyloid beta1-40 secretion by alphaLISA technique
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[PMID: 22225636] |
| HEK293 | IC50 |
0.25 μM
Compound: 2
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Inhibition of BACE1 in human HEK293 cells transfected with pCDNA-neo-SEAP-APP assessed as secreted alkaline phosphatase after cleavage of beta-site of APP by fluorescence assay
Inhibition of BACE1 in human HEK293 cells transfected with pCDNA-neo-SEAP-APP assessed as secreted alkaline phosphatase after cleavage of beta-site of APP by fluorescence assay
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[PMID: 20303626] |
| HEK-293T | IC50 |
29 nM
Compound: 2
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Inhibition of human BACE1 in HEK293T cells transfected with APP695 after 20 to 24 hrs by Western blot analysis
Inhibition of human BACE1 in HEK293T cells transfected with APP695 after 20 to 24 hrs by Western blot analysis
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[PMID: 20303626] |
| HEK-293T | EC50 |
43 nM
Compound: IV
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Inhibition of BACE1 expressed in HEK293T cells co-transfected APP with NFEV mutation at proteolytic site assessed as amyloid EV40 secretion
Inhibition of BACE1 expressed in HEK293T cells co-transfected APP with NFEV mutation at proteolytic site assessed as amyloid EV40 secretion
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[PMID: 22225636] |
| HEK-293T | IC50 |
29 nM
Compound: IV
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Inhibition of BACE1 expressed in HEK293T cells co-transfected APP with NFEV mutation at proteolytic site by sAPP_NF cell based assay
Inhibition of BACE1 expressed in HEK293T cells co-transfected APP with NFEV mutation at proteolytic site by sAPP_NF cell based assay
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[PMID: 22225636] |
| N2a | IC50 |
0.36 μM
Compound: IV
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Inhibition of beta amyloid 42 secretion in mouse N2a cells
Inhibition of beta amyloid 42 secretion in mouse N2a cells
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[PMID: 16821787] |
In the cell culture assay, β-Secretase Inhibitor IV (Compound 2) inhibits the production of Aβ peptides with an EC50 of 43 nM. β-Secretase Inhibitor IV potently suppresses the secretion of sAPP_NF and EV40 from HEK293T cells with an IC50 near 30 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 797035-11-1
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Appearance Solid
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Masse moléculaire 578.72
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Formule C31H38N4O5S
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Color White to light yellow
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SMILES
O=S(N(C)C1=CC(C(N[C@@H](CC2=CC=CC=C2)[C@H](O)CNC3CC3)=O)=CC(C(N[C@H](C)C4=CC=CC=C4)=O)=C1)(C)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
DMSO : 100 mg/mL (172.80 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.32 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (4.32 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureté et documentation
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Fiche technique (272 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.7280 mL | 8.6398 mL | 17.2795 mL | 43.1988 mL |
| 5 mM | 0.3456 mL | 1.7280 mL | 3.4559 mL | 8.6398 mL | |
| 10 mM | 0.1728 mL | 0.8640 mL | 1.7280 mL | 4.3199 mL | |
| 15 mM | 0.1152 mL | 0.5760 mL | 1.1520 mL | 2.8799 mL | |
| 20 mM | 0.0864 mL | 0.4320 mL | 0.8640 mL | 2.1599 mL | |
| 25 mM | 0.0691 mL | 0.3456 mL | 0.6912 mL | 1.7280 mL | |
| 30 mM | 0.0576 mL | 0.2880 mL | 0.5760 mL | 1.4400 mL | |
| 40 mM | 0.0432 mL | 0.2160 mL | 0.4320 mL | 1.0800 mL | |
| 50 mM | 0.0346 mL | 0.1728 mL | 0.3456 mL | 0.8640 mL | |
| 60 mM | 0.0288 mL | 0.1440 mL | 0.2880 mL | 0.7200 mL | |
| 80 mM | 0.0216 mL | 0.1080 mL | 0.2160 mL | 0.5400 mL | |
| 100 mM | 0.0173 mL | 0.0864 mL | 0.1728 mL | 0.4320 mL |
β-Secretase Inhibitor IV Related Classifications
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